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US5169428A - Tetrahydrophthalimide derivative and herbicide composition containing same - Google Patents

Tetrahydrophthalimide derivative and herbicide composition containing same Download PDF

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Publication number
US5169428A
US5169428A US07/726,724 US72672491A US5169428A US 5169428 A US5169428 A US 5169428A US 72672491 A US72672491 A US 72672491A US 5169428 A US5169428 A US 5169428A
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compound
tetrahydrophthalimide
methyl
hydrogen
derivative
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US07/726,724
Inventor
Kenji Tsuzuki
Sinzo Someya
Seigo Koura
Yasuaki Hanasaki
Mikio Ito
Hiroyuki Watanabe
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Tosoh Corp
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Tosoh Corp
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Priority claimed from JP62334000A external-priority patent/JP2542885B2/en
Priority claimed from JP62336451A external-priority patent/JP2542886B2/en
Priority claimed from JP63225465A external-priority patent/JPH0273066A/en
Priority claimed from JP63225463A external-priority patent/JPH0273064A/en
Priority claimed from JP63234258A external-priority patent/JPH0283368A/en
Application filed by Tosoh Corp filed Critical Tosoh Corp
Priority to US07/726,724 priority Critical patent/US5169428A/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/18Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
    • A01N37/32Cyclic imides of polybasic carboxylic acids or thio analogues thereof
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/36Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a singly bound oxygen or sulfur atom attached to the same carbon skeleton, this oxygen or sulfur atom not being a member of a carboxylic group or of a thio analogue, or of a derivative thereof, e.g. hydroxy-carboxylic acids
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/44Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
    • A01N37/46N-acyl derivatives
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N39/00Biocides, pest repellants or attractants, or plant growth regulators containing aryloxy- or arylthio-aliphatic or cycloaliphatic compounds, containing the group or, e.g. phenoxyethylamine, phenylthio-acetonitrile, phenoxyacetone
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/04Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
    • A01N43/06Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings
    • A01N43/08Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom five-membered rings with oxygen as the ring hetero atom
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/82Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms five-membered rings with three ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Definitions

  • This invention relates to a novel tetrahydrophthalimide derivative which has excellent herbicidal activity and selectivity.
  • the herbicidal activity of the tetrahydrophthalimide derivatives is well-known in the art.
  • Japanese Patent Disclosure (Kokai) Nos. 163365/82 and 110566/83 disclose the tetrahydrophthalimide derivatives having herbicidal activity, which are represented by the formula [A] and [B], respectively.
  • the known tetrahydrophthalimide derivatives do not have satisfactory herbicidal activity.
  • the other known tetrahydrophthalimide derivatives do not have satisfactory selectivity. That is, when the herbicide comprising the derivative is applied to the crops and weeds, not only the weeds, but also the crops may be damaged. Thus, the safety of the herbicide is not good.
  • the object of the present invention is to provide a novel tetrahydrophthalimide derivative which has a high herbicidal activity and selectivity.
  • Another object of the present invention is to provide a herbicide composition having a high herbicidal activity and selectivity.
  • the present inventors intensively studied to find that a specific tetrahydrophthalimide derivative has a high herbicidal activity and selectivity to complete the present invention.
  • the present invention provides a novel tetrahydrophthalimide derivative of the formula [I]: ##STR6## wherein X 1 and X 2 , the same or different, represent halogen, hydrogen or trifluoromethyl; R represents ##STR7## (wherein R 1 and R 2 , the same or different, represent hydrogen or methyl, R 3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadiazole-5-yl), ##STR8## (wherein R 4 is hydrogen or methyl, R 5 is methyl or benzyl), ##STR9## (wherein R 6 represents hydrogen or methyl, R 7 is halogen or C 1 -C 4 alkyl), (wherein R 8 is hydrogen, acyl or arylalkyl), cyano, or --CH 2 OR 9 (wherein R 9 is hydrogen, acetyl, halophenyl, C 1 -C 4 alkyl which may be substituted with alkoxycarbonyl).
  • the present invention a novel tetrahydrophthalimide derivative with high herbicidal activity and selectivity was provided As will be clearly demonstrated in the Examples later described, the tetrahydrophthalimide derivative of the present invention has a high herbicidal activity while it does not substantially damage the useful crops such as wheat, corn and soybean. Thus, it can be used safely for the inhibition of the growth of weeds in the field of such crops.
  • Preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] above include those represented by the following formula [II]: ##STR10##wherein R 1 and R 2 , the same or different, represent hydrogen or methyl, R 3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadiazol-5-yl.
  • Second group of the preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] includethose represented by the following formula [III]: ##STR15##wherein R 4 is hydrogen or methyl, R 5 is methyl or benzyl.
  • Third group of the preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] includethose represented by the following formula [IV]: ##STR18##wherein X 3 and X 4 , the same or different, represent halogen, R 6 represents hydrogen or methyl, R 7 represents halogen or C 1 -C 4 alkyl.
  • tetrahydrophthalimide derivative of the present invention is represented by the following formula [V]: ##STR19##wherein X 3 and X 4 , the same or different, represent halogen, R 8 represents hydrogen, acyl or arylalkyl.
  • tetrahydrophthalimide derivative of the present invention is represented by the following formula [VI]: ##STR22##wherein X 1 and X 2 , the same or different, represent hydrogen, halogen or trifluoromethyl, R 10 represents cyano or --CH 2 OR 9 (wherein R 9 represents hydrogen, acetyl, halophenyl, C 1 -C 4 alkyl which may be substituted with alkoxycarbonyl).
  • the tetrahydrophthalimide derivative of the present invention may be prepared by various processes. More particularly, those represented by theformula [II] may be prepared according to the following Equation 1: ##STR25##
  • Hal represents halogen (Hal means halogen also in the subsequent formulae)
  • R 1 , R 2 and R 3 represent the same meaning as in formula [II].
  • the reaction may be conducted in an appropriate solvent under the presence of a base at a temperature ranging from 0° C.-150° C., preferably 20°-100° C. for several minutes to 48 hours.
  • Preferred examples of the solvents which may be employed in the reaction may include ketones such as acetone and methyl ethyl ketone; aromatic hydrocarbons such as benzene and xylene; ethers such as ethyl ether, tetrahydrofuran and dioxane; halogenated hydrocarbons such as chlorobenzene, chloroform, tetrachloromethane and dichloroethane; tertiaryamines such as triethylamine, pyridine and dimethylaniline; and polar solvents such as acetonitrile, dimethylformamide, dimethylsulfoxide and hexamethylphosphoramide.
  • ketones such as acetone and methyl ethyl ketone
  • aromatic hydrocarbons such as benzene and xylene
  • ethers such as ethyl ether, tetrahydrofuran and dioxane
  • halogenated hydrocarbons such as chloro
  • the bases which may be employed in the reaction may include organic bases such as triethylamines, 1,3-diazabicyclo[5,4,0]undec-7-ene and dimethylaniline; alkali metal hydroxide such as sodium hydroxide; alkaline earth metal hydroxides such as calcium hydroxide; alkaline metal salts of carbonic acid such as sodiumcarbonate, potassium carbonate, sodium hydrogen carbonate and potassium hydrogen carbonate; and metal hydrides such as sodium hydride.
  • organic bases such as triethylamines, 1,3-diazabicyclo[5,4,0]undec-7-ene and dimethylaniline
  • alkali metal hydroxide such as sodium hydroxide
  • alkaline earth metal hydroxides such as calcium hydroxide
  • alkaline metal salts of carbonic acid such as sodiumcarbonate, potassium carbonate, sodium hydrogen carbonate and potassium hydrogen carbonate
  • metal hydrides such as sodium hydride.
  • tetrahydrophthalimide derivatives represented by the formula [III] may be prepared according to the following Equation 2 or 3: ##STR26##
  • the reaction may be conducted in the same conditions as in Equation 1.
  • the solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
  • tetrahydrophthalimide derivatives represented by the formula [IV] may be prepared according to the following Equation 4 or 5: ##STR27##
  • the reaction may be conducted in the same conditions as in Equation 1.
  • the solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
  • tetrahydrophthalimide derivatives represented by the formula [V] may beprepared according to the following Equation 6: ##STR28##
  • the reaction may be conducted in the same conditions as in Equation 1.
  • the solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
  • tetrahydrophthalimide derivatives represented by the formula [VI] may be prepared according to the following Equation 7 or 8: ##STR29##
  • the reaction according to the Equation 7 may be conducted in the same conditions as in Equation 1.
  • the solvents and bases which are preferred inEquation 1 are also preferred in these reactions.
  • the reaction according to the Equation 8 may be conducted in the presence or absence of a solvent, in the presence of a catalyst, at a temperature ranging from -20° C. to 300° C., preferably 0° C.-200° C. for several minutes to 48 hours.
  • Preferred examples of the catalysts which may be employed in the reaction of Equation 8 may include chlorinating agents or dehydrants such as phosphorus oxychloride, phosphorus pentoxide, phosphorus pentachloride, phosphorus trichloride and sulfuryl chloride; dehydrating reagents such astriethylamine, chloroformate, DCC and anhydrous acetic acid.
  • chlorinating agents or dehydrants such as phosphorus oxychloride, phosphorus pentoxide, phosphorus pentachloride, phosphorus trichloride and sulfuryl chloride
  • dehydrating reagents such astriethylamine, chloroformate, DCC and anhydrous acetic acid.
  • the amount of the catalyst is usually 1 to 100 equivalents with respect to 1 equivalent of the compound [XXI].
  • the present invention further provides a herbicide composition comprising the tetrahydrophthalimide derivative of the present invention as effectiveingredient in an agriculturally acceptable carrier.
  • the herbicide composition of the present invention is effective for inhibiting the growth of various weeds growing in paddy field including the weeds belonging to the Gramineae such as barnyardgrass; broadleaved weeds such as Falsepinpernel, spindle-flowered rotala, water starwart and monochoria;and those belonging to the family cyperaceae such as small flower umbrellaplant, slender spikerush and water nutgrass.
  • the tetrahydrophthalimide derivative of the present invention is particularly effective for inhibiting the growth of weeds growing in fields, such as mustard, virginia pepperweed, catchweed badstraw, Kinutaso (Galium kinuta), chick weed, Common lambsquaters, nottle (Utrica Thunbergiana), Common groundsel, Alender amaranth, Cocklebur, Pale smartweed, Velvetleaf and barynard grass.
  • the herbicide composition of the present invention does not substantially damage the crops belonging to Family Graminae such as corn, rice and wheat, so that it is highly safe.
  • liquid carrier or solid carrier may be employed.
  • liquid carrier ordiluent may include water, hydrocarbons, ethers, alkoxy alcohols, ketones, esters, amides and sulfoxides.
  • Preferred examples of the solid carriers orextender may include powder and granules of inorganic materials such as slaked lime, gypsum, calcium carbonate, silica, pearlite, pumice, diatomaceous earth, alumina, zeolite and clay minerals (e.g., talc, vermiculite and kaolinite); powder and granules of plant products such as starch, cereals and glucose; and powder and granules of synthetic productssuch as phenol resins, carbon resins and vinyl chloride resins.
  • the concentration of the active ingredient in the composition is not critical and may usually be 0.1% by weight to 90% by weight, preferably 1% by weight to 80% by weight.
  • the herbicide composition of the present invention may contain a surfactant.
  • the surfactants are well-known and widely used in the art.
  • Preferred examples of the surfactants include anion surfactants such as alkylsulfate esters, arylsulfonic acids, salts of succinic acid and polyethyleneglycolalkylaryl ethers and ester salts of sulfuric acid; cation surfactants such as alkylamines and polyoxyethylenealkylamines; non-ionic surfactants such as polyoxyethyleneglycol ethers and polyol esters; and ampholytic surfactants.
  • the herbicide composition of the present invention may contain other additives which are often employed in herbicide compositions.
  • the examples of such additives may include stabilizers, dispersion stabilizers, fixing agents, effect prolongers and synergists.
  • the composition may also contain other herbicides, bacteriocides, fungicides and the like.
  • the herbicide composition may be formulated to an emulsifiable concentrate,wettable powder, aqueous solution, oily solution, granule or powder.
  • the methods of formulating herbicide composition are well-known in the art.
  • This formulation may be prepared by uniformly mixing the components.
  • This composition may be prepared by mixing and pulverizing the components.
  • This composition may be prepared by mixing and pulverizing the components.
  • the amount of the compound of the present invention to be applied to the field varies depending on the formulation of the composition, method of application, species and stage of growth of the weeds. Typically, the amount to be applied may be 0.05 kg/ha to 10 kg/ha, preferably 0.1 kg/ha to 5 kg/ha in terms of the weight of the active compound of the present invention.
  • the herbicide composition of the present invention may directly be applied to the leaves or stems of weeds or to the field before the germination of the weeds.
  • the herbicide composition may be applied as it is or may be diluted with water before use.
  • Example 1 The same operation as in Example 1 was repeated except that a halogen compound [VIII]](see Equation 1) having methyl groups as R 1 and R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 1.
  • a halogen compound [VIII]] (see Equation 1) having methyl groups as R 1 and R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 1.
  • Example 2 The same operation as in Example 1 was repeated except that a halogen compound [VIII] (see Equation 1) having hydrogen as R 1 and methyl group as R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 2.
  • a halogen compound [VIII] (see Equation 1) having hydrogen as R 1 and methyl group as R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 2.
  • Example 1 The same operation as in Example 1 was repeated except that a halogen compound [VIII] (see Equation 1) having hydrogen as R 1 and R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 4.
  • a halogen compound [VIII] (see Equation 1) having hydrogen as R 1 and R 2 , and 3-methyl-1,2,4-oxadiazol-5-yl group as R 3 was used to obtain the Compound No. 4.
  • Example 5 The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 5-7. Further, for comparison, 5-[2-chloro-4-trifluoromethyl-phenoxy]-2-nitro-benzoic acid (Comparative Compound C) and the Comparative Compound A described in Example 5 were also tested. The results are shown in Table 7 below.
  • Example 9 The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 11-18. Further, for comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 9 below.
  • Example 21 The same procedure as in Example 21 was repeated except that the compounds tested were Compound No.s 19-23. For comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 10 below.
  • Example 5 The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 19-23. Further, for comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 11 below.
  • Example 31 The same procedure as in Example 31 was repeated except that N-(4-trifluoromethyl-5-aminocarbonylphenyl)-3,4,5,6-tetrahydrophthalimide was used to obtain the Compound No. 31.
  • Example 21 The same procedure as in Example 21 was repeated except that the compounds tested were Compound Nos. 24-30.
  • the Comparative Compound A described in Example 5 was also tested. The results are shown in Table 12 below.
  • Example 5 The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 24, 25, 27-31. Further, for comparison, the Comparative Compound A described in Example 5 was also tested. The resultsare shown in Table 13 below.

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Abstract

Disclosed is a tetrahydrophthalimide derivative of the formula (I): <IMAGE> [I] wherein X1 and X2, the same or different, represent halogen, hydrogen or trifluoromethyl; R represents <IMAGE> (wherein R1 and R2, the same or different, represent hydrogen or methyl, R3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadiazol-5-yl), <IMAGE> (wherein R4 is hydrogen or methyl, R5 is methyl or benzyl), <IMAGE> (wherein R6 represents hydrogen or methyl, R7 is halogen or C1 -C4 alkyl), <IMAGE> (wherein R8 is hydrogen, acyl or arylalkyl), cyano, or -CH2OR9 (wherein R9 is hydrogen, acetyl, halophenyl, C1-C4 tetrahydrophthalimide derivative of the present invention is useful as a herbicide.

Description

This is a continuation of application Ser. No. 07/291,759, filed Dec. 29, 1988, now abandoned.
BACKGROUND OF THE INVENTION
I. Field of the Invention
This invention relates to a novel tetrahydrophthalimide derivative which has excellent herbicidal activity and selectivity.
II. Description of the Related Art
The herbicidal activity of the tetrahydrophthalimide derivatives is well-known in the art. For example, Japanese Patent Disclosure (Kokai) Nos. 163365/82 and 110566/83 disclose the tetrahydrophthalimide derivatives having herbicidal activity, which are represented by the formula [A] and [B], respectively.
However, some of the known tetrahydrophthalimide derivatives do not have satisfactory herbicidal activity. The other known tetrahydrophthalimide derivatives do not have satisfactory selectivity. That is, when the herbicide comprising the derivative is applied to the crops and weeds, not only the weeds, but also the crops may be damaged. Thus, the safety of the herbicide is not good.
SUMMARY OF THE INVENTION
Accordingly, the object of the present invention is to provide a novel tetrahydrophthalimide derivative which has a high herbicidal activity and selectivity.
Another object of the present invention is to provide a herbicide composition having a high herbicidal activity and selectivity.
The present inventors intensively studied to find that a specific tetrahydrophthalimide derivative has a high herbicidal activity and selectivity to complete the present invention.
That is, the present invention provides a novel tetrahydrophthalimide derivative of the formula [I]: ##STR6## wherein X1 and X2, the same or different, represent halogen, hydrogen or trifluoromethyl; R represents ##STR7## (wherein R1 and R2, the same or different, represent hydrogen or methyl, R3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadiazole-5-yl), ##STR8## (wherein R4 is hydrogen or methyl, R5 is methyl or benzyl), ##STR9## (wherein R6 represents hydrogen or methyl, R7 is halogen or C1 -C4 alkyl), (wherein R8 is hydrogen, acyl or arylalkyl), cyano, or --CH2 OR9 (wherein R9 is hydrogen, acetyl, halophenyl, C1 -C4 alkyl which may be substituted with alkoxycarbonyl).
By the present invention, a novel tetrahydrophthalimide derivative with high herbicidal activity and selectivity was provided As will be clearly demonstrated in the Examples later described, the tetrahydrophthalimide derivative of the present invention has a high herbicidal activity while it does not substantially damage the useful crops such as wheat, corn and soybean. Thus, it can be used safely for the inhibition of the growth of weeds in the field of such crops.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
Preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] above include those represented by the following formula [II]: ##STR10##wherein R1 and R2, the same or different, represent hydrogen or methyl, R3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadiazol-5-yl.
Preferred and non-limiting specific examples of the tetrahydrophthalimide derivative represented by the formula [II]include those summarized in Table 1 below.
              TABLE 1                                                     
______________________________________                                    
Compound No. R.sup.1  R.sup.2 R.sup.3                                     
______________________________________                                    
1            CH.sub.3 CH.sub.3                                            
                               ##STR11##                                  
2            H        CH.sub.3                                            
                               ##STR12##                                  
3            CH.sub.3 H                                                   
                               ##STR13##                                  
4            H        H                                                   
                               ##STR14##                                  
______________________________________                                    
Second group of the preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] includethose represented by the following formula [III]: ##STR15##wherein R4 is hydrogen or methyl, R5 is methyl or benzyl.
Preferred and non-limiting specific examples represented by the formula [III]include those summarized in Table 2 below.
              TABLE 2                                                     
______________________________________                                    
Compound No.   R.sup.4   R.sup.5                                          
______________________________________                                    
5              CH.sub.3  CH.sub.3                                         
6              H                                                          
                          ##STR16##                                       
7              CH.sub.3                                                   
                          ##STR17##                                       
______________________________________                                    
Third group of the preferred examples of the tetrahydrophthalimide derivative of the present invention represented by the formula [I] includethose represented by the following formula [IV]: ##STR18##wherein X3 and X4, the same or different, represent halogen, R6 represents hydrogen or methyl, R7 represents halogen or C1 -C4 alkyl.
Preferred and non-limiting specific examples represented by the formula [IV]include those summarized in Table 3 below.
              TABLE 3                                                     
______________________________________                                    
Compound No.  R.sup.6  X.sup.3                                            
                             X.sup.4 R.sup.7                              
______________________________________                                    
8             H        H     Cl      --                                   
9             H        H     Cl      2-F                                  
10            H        H     Cl      4-F                                  
11            H        F     Cl      --                                   
12            H        F     Cl      2-F                                  
13            H        F     Cl      2-CH.sub.3                           
14            H        Cl    Cl      2-F                                  
15            H        Br    Cl      --                                   
16            H        Br    Cl      2-F                                  
17            CH.sub.3 F     Cl      --                                   
18            CH.sub.3 Cl    Cl      --                                   
______________________________________                                    
Fourth group of preferred examples of the tetrahydrophthalimide derivative of the present invention is represented by the following formula [V]: ##STR19##wherein X3 and X4, the same or different, represent halogen, R8 represents hydrogen, acyl or arylalkyl.
Preferred and non-limiting specific examples of those represented by the formula [V] include those summarized in Table 4 below.
              TABLE 4                                                     
______________________________________                                    
Compound No. X.sup.3                                                      
                    X.sup.4   R.sup.8                                     
______________________________________                                    
19           F      Cl        H                                           
20           F      Cl        COCH.sub.3                                  
21           F      Cl                                                    
                               ##STR20##                                  
22           Cl     Cl                                                    
                               ##STR21##                                  
23           Cl     Cl        H                                           
______________________________________                                    
Fifth group of preferred examples of the tetrahydrophthalimide derivative of the present invention is represented by the following formula [VI]: ##STR22##wherein X1 and X2, the same or different, represent hydrogen, halogen or trifluoromethyl, R10 represents cyano or --CH2 OR9 (wherein R9 represents hydrogen, acetyl, halophenyl, C1 -C4 alkyl which may be substituted with alkoxycarbonyl).
Preferred and non-limiting specific examples of those represented by the formula [VI] are summarized in Table 5 below.
              TABLE 5                                                     
______________________________________                                    
Compound No. X.sup.1 X.sup.2 R.sup.8                                      
______________________________________                                    
24           H       Cl      CH.sub.2 OH                                  
25           H       Cl      CH.sub.2 OCOCH.sub.3                         
26           H       Cl                                                   
                              ##STR23##                                   
27           H       Cl                                                   
                              ##STR24##                                   
28           H       Cl      CN                                           
29           H       Br      CN                                           
30           F       Cl      CN                                           
31           H       CF.sub.3                                             
                             CN                                           
______________________________________                                    
The tetrahydrophthalimide derivative of the present invention may be prepared by various processes. More particularly, those represented by theformula [II] may be prepared according to the following Equation 1: ##STR25##
In the above Equation 1, Hal represents halogen (Hal means halogen also in the subsequent formulae), R1, R2 and R3 represent the same meaning as in formula [II].
The reaction may be conducted in an appropriate solvent under the presence of a base at a temperature ranging from 0° C.-150° C., preferably 20°-100° C. for several minutes to 48 hours.
Preferred examples of the solvents which may be employed in the reaction may include ketones such as acetone and methyl ethyl ketone; aromatic hydrocarbons such as benzene and xylene; ethers such as ethyl ether, tetrahydrofuran and dioxane; halogenated hydrocarbons such as chlorobenzene, chloroform, tetrachloromethane and dichloroethane; tertiaryamines such as triethylamine, pyridine and dimethylaniline; and polar solvents such as acetonitrile, dimethylformamide, dimethylsulfoxide and hexamethylphosphoramide.
Preferred examples of the bases which may be employed in the reaction may include organic bases such as triethylamines, 1,3-diazabicyclo[5,4,0]undec-7-ene and dimethylaniline; alkali metal hydroxide such as sodium hydroxide; alkaline earth metal hydroxides such as calcium hydroxide; alkaline metal salts of carbonic acid such as sodiumcarbonate, potassium carbonate, sodium hydrogen carbonate and potassium hydrogen carbonate; and metal hydrides such as sodium hydride.
Typically, 1-5 equivalents of the halogen compound [VIII] and 1-10 equivalents of the base are reacted with 1 equivalent of the compound [VII].
The tetrahydrophthalimide derivatives represented by the formula [III] may be prepared according to the following Equation 2 or 3: ##STR26##
The reaction may be conducted in the same conditions as in Equation 1. The solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
Typically, 1-5 equivalents of the compound [X] or [XII] and 1-10 equivalents of the base are reacted with 1 equivalent of the compound [IX]or [XI].
The tetrahydrophthalimide derivatives represented by the formula [IV] may be prepared according to the following Equation 4 or 5: ##STR27##
The reaction may be conducted in the same conditions as in Equation 1. The solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
Typically, 1-5 equivalents of the compound [XIV] or [XVI] and 1-10 equivalents of the base are reacted with 1 equivalent of the compound [XIII] or [XV].
The tetrahydrophthalimide derivatives represented by the formula [V] may beprepared according to the following Equation 6: ##STR28##
The reaction may be conducted in the same conditions as in Equation 1. The solvents and bases which are preferred in Equation 1 are also preferred inthese reactions.
Typically, 1-5 equivalents of the compound [XVIII] and 1-10 equivalents of the base are reacted with 1 equivalent of the compound [XVII].
The tetrahydrophthalimide derivatives represented by the formula [VI] may be prepared according to the following Equation 7 or 8: ##STR29##
The reaction according to the Equation 7 may be conducted in the same conditions as in Equation 1. The solvents and bases which are preferred inEquation 1 are also preferred in these reactions.
Typically, 1-5 equivalents of the compound [XX] and 1-10 equivalents of thebase are reacted with 1 equivalent of the compound [XIX].
The reaction according to the Equation 8 may be conducted in the presence or absence of a solvent, in the presence of a catalyst, at a temperature ranging from -20° C. to 300° C., preferably 0° C.-200° C. for several minutes to 48 hours.
The solvents preferred in the reaction of Equation 1 are also preferred in the reaction of Equation 8.
Preferred examples of the catalysts which may be employed in the reaction of Equation 8 may include chlorinating agents or dehydrants such as phosphorus oxychloride, phosphorus pentoxide, phosphorus pentachloride, phosphorus trichloride and sulfuryl chloride; dehydrating reagents such astriethylamine, chloroformate, DCC and anhydrous acetic acid.
The amount of the catalyst is usually 1 to 100 equivalents with respect to 1 equivalent of the compound [XXI].
The present invention further provides a herbicide composition comprising the tetrahydrophthalimide derivative of the present invention as effectiveingredient in an agriculturally acceptable carrier. The herbicide composition of the present invention is effective for inhibiting the growth of various weeds growing in paddy field including the weeds belonging to the Gramineae such as barnyardgrass; broadleaved weeds such as Falsepinpernel, spindle-flowered rotala, water starwart and monochoria;and those belonging to the family cyperaceae such as small flower umbrellaplant, slender spikerush and water nutgrass. Further, the tetrahydrophthalimide derivative of the present invention is particularly effective for inhibiting the growth of weeds growing in fields, such as mustard, virginia pepperweed, catchweed badstraw, Kinutaso (Galium kinuta), chick weed, Common lambsquaters, nottle (Utrica Thunbergiana), Common groundsel, Alender amaranth, Cocklebur, Pale smartweed, Velvetleaf and barynard grass. The herbicide composition of the present invention does not substantially damage the crops belonging to Family Graminae such as corn, rice and wheat, so that it is highly safe.
The agriculturally acceptable carriers per se which may be employed in the present invention are well-known in the art, and either liquid carrier or solid carrier may be employed. Preferred examples of the liquid carrier ordiluent may include water, hydrocarbons, ethers, alkoxy alcohols, ketones, esters, amides and sulfoxides. Preferred examples of the solid carriers orextender may include powder and granules of inorganic materials such as slaked lime, gypsum, calcium carbonate, silica, pearlite, pumice, diatomaceous earth, alumina, zeolite and clay minerals (e.g., talc, vermiculite and kaolinite); powder and granules of plant products such as starch, cereals and glucose; and powder and granules of synthetic productssuch as phenol resins, carbon resins and vinyl chloride resins. The concentration of the active ingredient in the composition is not critical and may usually be 0.1% by weight to 90% by weight, preferably 1% by weight to 80% by weight.
If necessary, the herbicide composition of the present invention may contain a surfactant. The surfactants are well-known and widely used in the art. Preferred examples of the surfactants include anion surfactants such as alkylsulfate esters, arylsulfonic acids, salts of succinic acid and polyethyleneglycolalkylaryl ethers and ester salts of sulfuric acid; cation surfactants such as alkylamines and polyoxyethylenealkylamines; non-ionic surfactants such as polyoxyethyleneglycol ethers and polyol esters; and ampholytic surfactants. If desired, the herbicide composition of the present invention may contain other additives which are often employed in herbicide compositions. The examples of such additives may include stabilizers, dispersion stabilizers, fixing agents, effect prolongers and synergists. The composition may also contain other herbicides, bacteriocides, fungicides and the like.
The herbicide composition may be formulated to an emulsifiable concentrate,wettable powder, aqueous solution, oily solution, granule or powder. The methods of formulating herbicide composition are well-known in the art.
Specific non-limiting examples of the preferred formulations of the presentinvention will now be described. In the following examples, all parts are based on weight.
______________________________________                                    
Formulation 1 (Emulsifiable Concentrate)                                  
______________________________________                                    
Compound of the present invention:                                        
                         20    parts                                      
xylene:                  60    parts                                      
Solpol (a surfactant commercially                                         
                         20    parts                                      
available from Toho Kogaku Kogyo)                                         
______________________________________                                    
This formulation may be prepared by uniformly mixing the components.
______________________________________                                    
Formulation 2 (Wettable Powder)                                           
______________________________________                                    
Compound of the present invention                                         
                         20    parts                                      
White Carbon             10    parts                                      
Zeaklite                 65    parts                                      
Solpol (a surfactant commercially                                         
                         5     parts                                      
available from Toho Kogaku Kogyo)                                         
______________________________________                                    
This composition may be prepared by mixing and pulverizing the components.
______________________________________                                    
Formulation 3 (Wettable Powder)                                           
______________________________________                                    
Compound of the present invention                                         
                         10    parts                                      
Zeaklite                 87    parts                                      
Neoplex Powder (commercially                                              
                         1.5   parts                                      
available from Kao corporation)                                           
Solpol (a surfactant commercially                                         
                         1.5   parts                                      
available from Toho Kogaku Kogyo)                                         
______________________________________                                    
This composition may be prepared by mixing and pulverizing the components.
The amount of the compound of the present invention to be applied to the field varies depending on the formulation of the composition, method of application, species and stage of growth of the weeds. Typically, the amount to be applied may be 0.05 kg/ha to 10 kg/ha, preferably 0.1 kg/ha to 5 kg/ha in terms of the weight of the active compound of the present invention.
The herbicide composition of the present invention may directly be applied to the leaves or stems of weeds or to the field before the germination of the weeds. The herbicide composition may be applied as it is or may be diluted with water before use.
The invention will now be described by way of the examples thereof. It should be understood that the examples are presented for the illustration purpose only and should not be interpreted any restrictive way.
EXAMPLE 1 Preparation of N-[4-chloro-2-fluoro-5-(1-tetrahydrofurfuryloxycarbonyl)-ethoxyphenyl-2,4,5,6 -tetrahydrophthalimide (Compound No. 3 (see Table 1)
To 20 ml of acetonitrile containing 0.59 g of N-(4-chloro-2-fluoro-5-hydroxyphenyl)3,4,5,6-tetrahydrophthalimide and 0.30 g of anhydrous potassium carbonate, was added 0.30 g of 2-chloropropionic acid tetrahydrofurfuryl ester in 10 ml of acetnitrile and the resulting mixture was heated to reflux for 5 hours. After allowingto cool, water was added to the mixture and the resulting mixture was extracted with ether. After drying the extract, the solvent was evaporatedunder reduced pressure and the obtained residue was subjected to a column chromatography (silica gel) to obtain 0.65 g of oily product. The eluant employed in the column chromatography was chloroform/ethyl acetate=10/1 (v/v).
1 H-NMR (60 MHz, CDCl3 solvent) δppm 1.5-1.9 (m, 11H), 2.1-2.5 (m, 4H), 3.4-4.3 (m, 5H), 4.76 (q, J=7 Hz, 1H), 6.86 (dd, J=1.5, 6Hz, 1H), 7.28 (d, J=9 Hz, 1H)
Refractive Index (dD 25): 1.5448
EXAMPLE 2 Preparation of Compound No. 1 (Table 1)
The same operation as in Example 1 was repeated except that a halogen compound [VIII]](see Equation 1) having methyl groups as R1 and R2, and 3-methyl-1,2,4-oxadiazol-5-yl group as R3 was used to obtain the Compound No. 1.
1 H-NMR (60 mHz, CDCl3 solvent) δppm 1.5-2.0 (m, 10H), 2.2-2.6 (m, 7H), 4.83 (q, J=7 Hz, 1H), 6.05 (q, J=7 Hz, 1H), 6.81 (t, J=6 Hz, 1H), 7.25 (d, J=9 Hz, 1H)
Refractive Index (nD 25): 1.5382
EXAMPLE 3 Preparation of Compound No. 2 (Table 1)
The same operation as in Example 1 was repeated except that a halogen compound [VIII] (see Equation 1) having hydrogen as R1 and methyl group as R2, and 3-methyl-1,2,4-oxadiazol-5-yl group as R3 was used to obtain the Compound No. 2.
1 H-NMR (60 MHz, CDCl3 solvent) δppm 1.70 (d, J=7 Hz, 3H), 1.6-2.0 (m, 4H), 2.36 (s, 3H), 2.2-2.6 (m, 4H), 4.76 (s, 2H), 6.10 (q, J=7Hz, 1H), 6.83 (d, J=6 Hz, 1H), 7.25 (d, J=9 Hz, 1H)
Refractive Index (nD 25): 1.5503
EXAMPLE 4 Preparation of Compound No. 4 (Table 1)
The same operation as in Example 1 was repeated except that a halogen compound [VIII] (see Equation 1) having hydrogen as R1 and R2, and 3-methyl-1,2,4-oxadiazol-5-yl group as R3 was used to obtain the Compound No. 4.
1 H-NMR (60 MHz, CDCl3 solvent) δppm 1.5-1.9 (m, 4H0, 2.30 (s, 3H), 2.1-2.5 (m, 4H), 4.75 (s, 2H), 5.30 (s, 2H), 6.80 (d, J=6 Hz, 1H), 7.20 (d, J=9 Hz, 1H)
Refractive Index (nD 25): 1.5407
EXAMPLE 5 Test for Evaluation of Effectiveness in Growth Inhibition by Foliage Treatment
Field soil was packed in a plastic vat sizing 22 cm×16 cm and seeds of wheat (Triticum aestivum), corn (Zea mays) and soybean (Glycine max) were sown. The field soil was covered with soil of about 1 cm thickness which contains seeds of weeds, i.e., barnyardgrass (Echinochloa crus-galli), Velvetleaf, Slender amaranth, Cocklebur and Pale smartweed. When the barnyardgrass grew to have 2-2.5 leaves, each of the Compound Nos. 1-3 of the present invention was applied in the amount shown in Table6 below. Further, for comparison, the compound of the formula [A] disclosedin Japanese Patent Disclosure (Kokai) No. 163365/82 (comparative compound A) and the compound of the formula [B] disclosed in Japanese Patnt Disclosure (Kokai) No. 110566/83 (comparative compound B) were applied separately. After 14 days from the application of the herbicide, the conditions of the growth of the weeds and the crops were observed. The results are shown in Table 6. The herbicidal effectiveness was rated in 6ranks as follows:
Rank 0: percent growth inhibition of 0-9%
Rank 1: percent growth inhibition of 10-29%
Rank 2: percent growth inhibition of 30-49%
Rank 3: percent growth inhibition of 50-69%
Rank 4: percent growth inhibition of 70-89%
Rank 5: percent growth inhibition of 90-100%
                                  TABLE 6                                 
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              Herbicidal Effectiveness                                    
        Rate  Barnyard-                                                   
                    Pale  Slender          Phytotoxicity                  
Compound No.                                                              
        (a.i. g/10a)                                                      
              grass smartweed                                             
                          amaranth                                        
                               Cocklebur                                  
                                     Velvetleaf                           
                                           Wheat                          
                                               Corn                       
                                                  Soybean                 
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1       60    1     5     5    5     5     0   0  0                       
        125   1     5     5    5     5     0   0  0                       
2       60    0     5     5    5     5     0   0  0                       
        125   3     5     5    5     5     0   0  0                       
3       60    4     2     5    5     5     0   0  0                       
        125   4     5     5    5     5     0   0  0                       
Comparative                                                               
        60    2     5     5    5     5     2   2  4                       
Compound A                                                                
        125   4     5     5    5     5     3   2  5                       
Comparative                                                               
        60    5     5     5    5     5     0   2  2                       
Compound B                                                                
        125   5     5     5    5     5     2   2  3                       
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EXAMPLE 6 Preparation of N-[4-chloro-2-fluoro-5-{(3-methyl-1,2,4-oxadiazo-5-yl)-1-ethyloxy}phenyl]-3,4,5,6-tetrahydrophthalimide (Compound No. 5, (Table 2))
To 50 ml of acetonitrile, 0.6 g of 3-methyl-5-(chloroethyl)-1,2,4-oxadiazole, 1.12 g of N-(4-chloro-2-fluoro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide and 0.58 g of potassium carbonate were added and the mixture was heated to reflux for 16 hours. After the reaction mixture was allowed to cool, inorganic materials were removed by filtration and acetonitrile was evaporated. The residue was purified by column chromatography (silica gel)to obtain 0.72 g of the desired product. The eluant employed in the column chromatography was benzene/ethyl acetate=10/1 (v/v).
1 H-NMR (60 MHz, CDCl3 solvent) δppm 1.83 (d, J=7 Hz, 3H), 1.6-2.0 (m, 4H), 2.40 (s, 3H), 2.2-2.6 (m, 4H), 5.47 (q, J=7 Hz, 1H), 6.90(d, J=6 Hz, 1H) 7.24 (d, J=9 Hz, 1H)
m.p.: 95°-97.5° C.
EXAMPLE 7 Preparation of N-[4-chloro-2-fluoro-5-{(3-benzyl-1,2,4-oxadiazo-5-yl)methyloxy}phenyl]-3,4,5,6-tetrahydrophthalimide (Compound No. 6, (Table 2))
To 50 ml of acetic acid, 1.67 g of 4-chloro-2-fluoro-5-(3-benzyl-1,2,4-oxadiazol-5-yl)methyloxyaniline and 0.76 g of 3,4,5,6-tetrahydrophthalic anhydride were added, and the mixturewas heated to reflux for 16 hours under stirring The reaction mixture was then concentrated under reduced pressure and under heat, and the residue was purified by column chromatography (silica gel) to obtain 1.73 g of thedesired product. The eluant employed in the column chromatography was benzene/ethyl acetate=10/1 (v/v).
1 H-NMR (60 MHz CDCl3 solvent) δppm 1.4-1.9 (m, 4H, 2.0-2.5(m, 4H), 4.42 (s, 2H), 5.03 (s, 2H), 5.03 (s, 2H), 6.80 (d, J=6 Hz, 1H), 6.9-7.3 (broad s, 6H)
Refractive Index (nD 25) 1.5761
EXAMPLE 8 Preparation of Compound No. 7 (Table 2)
The same operation as in Example 7 was repeated except that the compound [X] in Equation 2 had methyl group as R4 to obtain the Compound No. 7.
1 H-NMR (60 MHz, CDCl3 solvent δppm 1.83 (d, J=7 Hz, 3H), 1.6-2.0 (m, 4H), 2.2-2.6 (m, 4H), 4.11 (s, 2H), 5.43 (q, J=7 Hz, 1H), 6.88(d, J=6 Hz, 1H), 7.1-7.4 (m, 6H)
Refractive Index (nD 25) 1.5708
EXAMPLE 9 Test for Evaluation of Effectiveness in Growth Inhibition by Foliage Treatment
The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 5-7. Further, for comparison, 5-[2-chloro-4-trifluoromethyl-phenoxy]-2-nitro-benzoic acid (Comparative Compound C) and the Comparative Compound A described in Example 5 were also tested. The results are shown in Table 7 below.
                                  TABLE 7                                 
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              Herbicidal Effectiveness                                    
        Rate  Barnyard-                                                   
                    Pale  Slender          Phytotoxicity                  
Compound No.                                                              
        (a.i. g/10a)                                                      
              grass smartweed                                             
                          amaranth                                        
                               Cocklebur                                  
                                     Velvetleaf                           
                                           Wheat                          
                                               Corn                       
                                                  Soybean                 
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5       15    3     5     5    5     5     0   0  0                       
        30    4     5     5    5     5     0   0  0                       
6       15    3     5     5    5     5     0   0  0                       
        30    5     5     5    5     5     0   0  0                       
7       15    4     5     5    5     5     0   0  0                       
        30    4     5     5    5     5     0   0  0                       
Comparative                                                               
        15    0     5     5    4     3     0   0  3                       
Compound C                                                                
        30    3     5     5    4.5   4.5   2   2  4                       
Comparative                                                               
        15    0     5     4.5  4.5   5     0   0  4.5                     
Compound A                                                                
        30    0     5     5    5     5     1   1  5                       
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EXAMPLE 10 Preparation of N-(5-benzyloxy-4-chlorophenyl-3,4,5,6-tetrahydrophthalimide (Compound No. 8 (Table 3))
To 50 ml of acetonitrile, 0.55 g of N-(4-chloro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide, 0.38 g of benzyl bromide and 0.27 g of potassium carbonate were added and the mixture was heated to reflux under stirring After cooling, the inorganic materials were removed by filtration and the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (silica gel, benzene/ethyl acetate=10/1 (v/v)) to obtain 0.6 g of the desired product.
Refractive Index nD 25 : 1.5909
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  68.83        4.97   3.82                                       
Calcd. (%) 68.57        4.93   3.80                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.80 (mc, 4H), 2.40 (mc, 4H), 4.92 (s, 2H), 7.20 (mc, 8H)
EXAMPLE 11 Preparation of N-(2,4-dichloro-5-(2-fluorophenyloxy)phenyl-3,4,5,6-tetrahydrophthalimide (Compound No. 14 (Table 3))
To 50 ml of acetic acid, 0.43 g of 3,4,5,6-tetrahydrophthalic anhydride and0.80 g of 2,4-dichloro-5-aminophenyl-2'-fluorobenzyl ether were added and the mixture was heated to reflux for 16 hours under stirring. After cooling, the solvent was evaporated under reduced pressure and the residuewas purified by column chromatography (silica gel, benzene/ethyl acetate=10/1 (v/v)) to obtain 0.7 g of the desired product.
m.p.: 106°-108.5° C.
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  59.8         3.81   3.36                                       
Calcd. (%) 60.01        3.83   3.33                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.70 (mc, 4H), 2.33 (mc, 4H), 5.07 (s, 3H), 7.22 (mc, 6H)
EXAMPLE 12 Preparation of Compound No. 9
To 50 ml of acetonitrile, 0.43 g of N-(4-chloro-5-hydroxyphenyl)-3,4,5,6-tetraphydrophthalimide, 0.3 g of 2-fluoro-benzyl bromide and 0.21 g of potassium carbonate were added and the same procedure as in Example 10 was followed to obtain 0.62 g of the Compound No. 9.
m.p.: 88.5°-91° C.
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  65.71        4.27   3.31                                       
Calcd. (%) 65.37        4.44   3.63                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.78 (mc, 4H), 2.42 (mc, 4H), 5.10 (s, 2H), 7.20 (mc, 7H)
EXAMPLE 13 Preparation of Compound No. 10
To 50 ml of acetonitrile, 0.55 g of N-(4-chloro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide, 0.38 g of 4-fluoro-benzyl bromide and 0.27 g of potassium carbonate were added and the same procedure as in Example 10 was followed to obtain 0.7 g of the Compound No. 10.
Refractive Index nD : 1.5730
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  64.99        4.52   3.98                                       
Calcd. (%) 65.37        4.44   3.63                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.74 (mc, 4H), 2.40 (mc, 4H), 4.92 (s, 2H), 7.10 (mc, 8H)
EXAMPLE 14 Preparation of Compound No. 11
To 50 ml of acetonitrile, 0.46 g anhydrous N-(4-chloro-2-fluoro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimidic acid,0.27 g of benzyl bromide and 0.21 g of potassium carbonate were added and the same procedure as in Example 10 was followed to obtain 0.69 g of the Compound No. 11.
Refractive Index nD 25 : 1.5968
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  65.22        4.58   3.59                                       
Calcd. (%) 65.37        4.44   3.63                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.75 (mc, 4H), 2.38 (mc, 4H), 5.03 (s, 2H), 7.28 (mc, 7H)
EXAMPLE 15 Preparation of Compound No. 12
To 50 ml of acetonitrile, 1.0 g of N-(4-chloro-2-fluoro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide, 0.6 gof 2-fluoro-benzyl chloride and 0.56 g of potassium carbonate were added and the same procedure as in Example 10 was followed to obtain 1.02 g of the Compound No. 12.
m.p.: 93°-95° C.
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  62.33        4.06   3.42                                       
Calcd. (%) 62.46        3.99   3.46                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.70 (mc, 4H), 2.33 (mc, 4H), 5.08 (s, 2H), 7.22 (mc, 6H)
EXAMPLE 16 Preparation of Compound No. 13
To 50 ml of acetonitrile, 0.46 g of N-(4-chloro-2-fluoro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide, 0.29 g of 2-methyl-benzyl bromide and 0.21 g of potassium carbonate were added and the same procedure as in Example 10 was followed to obtain 0.67 g of the Compound No. 13.
m.p.: 135°-137° C.
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  66.12        4.67   3.2                                        
Calcd. (%) 66.08        4.78   3.5                                        
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.82 (mc, 4H), 2.33 (s, 3H), 2.38 (mc, 4H), 5.17 (s, 2H), 7.13 (mc, 6H)
EXAMPLE 17 Preparation of Compound 15
To 50 ml of acetonitrile, 0.75 g of N-(2-bromo-4-chloro-5-hydroxyphenyl)-3,4,5,6-tetrahydrophthalimide, 0.36 gof benzyl bromide and 0.29 g of potassium carbonate were added and the sameprocedure as in Example 10 was followed to obtain 0.57 g of the Compound No. 15.
Refractive Index: nD 25 : 1.5839
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  56.55        3.7    3.23                                       
Calcd. (%) 56.46        3.83   3.13                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.67 (mc, 4H), 2.30 (mc, 4H), 5.03 (s, 2H), 7.17 (mc, 7H)
EXAMPLE 18 Preparation of Compound No 16
To 50 ml of acetic acid, 0.76 g of 3,4,5,6-tetrahydrophthalic anhydride and1.7 g of 2-bromo-4-chloro-5-aminophenyl-2'-fluorobenzyl ether were added and the same procedure as in Example 11 was followed to obtain 1.72 g of the Compound No. 16.
m.p.: 142°-144.5° C.
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  54.44        3.29   2.77                                       
Calcd. (%) 54.27        3.47   3.01                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.70 (mc, 4H), 2.30 (mc, 4H), 5.10 (s, 2H), 7.19 (mc, 7H)
EXAMPLE 19 Preparation of Compound No. 17
To 50 ml of acetic acid, 0.76 g of 3,4,5,6-tetrahydrophthalic anhydride and1.35 g of 4-chloro-2-fluoro-5-aminophenyl-(1-phenyl)-ethyl ether were addedand the same procedure as in Example 11 was followed to obtain 1.25 g of the Compound No. 17.
Refractive Index:nD 25 : 1.5509
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  66.06        4.85   3.44                                       
Calcd. (%) 66.08        4.78   3.5                                        
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.42 (d, 3H), 2.30 (mc, 4H), 2.35 (mc, 4H), 4.80 (q, 1H), 6.79 (mc, 7H)
EXAMPLE 20
To 50 ml of acetic acid, 0.76 g of 3,4,5,6-tetrahydrophthalic anhydride and1.92 g of 2,4-dichloro-5-aminophenyl-(1-phenyl)-ethyl ether were added and the same procedure as in Example 11 was followed to obtain 1.48 g of the Compound No. 18.
Refractive Index:nD 25 : 1.5509
______________________________________                                    
Element Analysis                                                          
         C          H      N                                              
______________________________________                                    
Found (%)  63.65        4.58   3.27                                       
Calcd. (%) 63.47        4.6    3.36                                       
______________________________________                                    
1 H-NMR (CDCl3, δppm) 1.63 (d, 3H), 1.75 (mc, 4H), 2.33 (mc, 4H), 5.28 (q, 1H), 7.00 (mc, 7H)
EXAMPLE 21 Test for Evaluation of Effectiveness in Growth Inhibition by Soil Treatment
Paddy field soil was packed in a plastic pot with 60 cm diameter. After puddling, the seeds of weeds shown in Table 8 below were sown and one seedling of rice (variety: Yamahoshi) with 2 leaves were transplanted. Thewater level was kept at about 3 cm above the soil. The herbicide compositions formulated according to the above-described Formulation 3 wasdiluted with water and was uniformly applied to the water surface in the amount shown in Table 8. Further, for comparison, N-4-chloro-2-fluoro-5-isopropoxyphenyl)2-ethoxycarbonylcyclohexyl carboxylic acid ethyl ester (Comparative Compound D) disclosed in JapanesePatent Disclosure (Kokai) No. 33154/86 was also tested. After 20 days from the application of the herbicide, the growing conditions of the weeds and the rice were observed. The growth inhibition was rated in 6 ranks as in Example 5. The results are shown in Table 8.
                                  TABLE 8                                 
__________________________________________________________________________
                                      Annual                              
        Rate     Barnyard-                                                
                       Small flower   broadleaved                         
Compound No.                                                              
        (a.i. g/10a)                                                      
              Rice                                                        
                 grass unbrellaplant                                      
                               Monochoria                                 
                                      weeds                               
__________________________________________________________________________
8       250   0  3     5       5      5                                   
        125   0  3     5       5      5                                   
        60    0  3     5       5      5                                   
9       250   0  0     5       5      5                                   
        125   0  0     5       5      5                                   
        60    0  0     5       5      5                                   
10      250   0  0     4       5      5                                   
        125   0  0     4       5      5                                   
        60    0  0     3       5      5                                   
11      125   1  5     5       5      5                                   
        60    0  5     5       5      5                                   
        30    0  5     5       5      5                                   
12      125   0  5     5       5      5                                   
        60    0  5     5       5      5                                   
        30    0  5     5       5      5                                   
13      125   0  4     5       5      5                                   
        60    0  4     5       5      5                                   
        30    0  4     5       5      5                                   
14      250   0  2     5       5      5                                   
        125   0  0     5       4      5                                   
        60    0  0     4       4      5                                   
15      125   0  4     5       5      5                                   
        60    0  4     5       5      5                                   
        30    0  4     5       5      5                                   
16      250   0  4     5       5      5                                   
        125   0  4     5       4      5                                   
        60    0  3     5       4      5                                   
17      125   0  5     5       5      5                                   
        60    0  5     5       5      5                                   
        30    0  4     5       5      5                                   
18      125   0  4     5       5      5                                   
        60    0  3     5       5      5                                   
        30    0  3     5       5      5                                   
Comparative                                                               
        125   0  0     2       0      0                                   
Compound D                                                                
        60    0  0     0       0      0                                   
        30    0  0     0       0      0                                   
__________________________________________________________________________
EXAMPLE 22 Test for Evaluation of Effectiveness in Growth Inhibition by Foliage Treatment
The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 11-18. Further, for comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 9 below.
                                  TABLE 9                                 
__________________________________________________________________________
        Rate              Slender                                         
Compound No.                                                              
        (a.i. g/10a)                                                      
              Soybean                                                     
                   Wheat                                                  
                       Corn                                               
                          amaranth                                        
                               Velvetleaf                                 
                                     Cocklebur                            
__________________________________________________________________________
11      125   1    0   1  5    5     5                                    
        60    1    0   0  5    5     5                                    
        30    0    0   0  5    5     5                                    
12      125   1    0   0  5    5     5                                    
        60    0    0   0  5    5     5                                    
        30    0    0   0  5    5     4.5                                  
13      125   1    0   1  5    5     4.5                                  
        60    0    0   0  5    4.5   4                                    
        30    0    0   0  5    4.5   3                                    
15      125   2    0   0  5    5     4.5                                  
        60    1    0   0  5    4.5   3                                    
        30    1    0   0  5    4.5   3                                    
16      125   1    0   0  4    4     3                                    
        60    0    0   0  4    3     3                                    
        30    0    0   0  3    3     0                                    
17      125   3    2   1  5    5     5                                    
        60    3    2   1  5    5     5                                    
        30    2    1   0  5    5     4.5                                  
18      125   1    0   0  5    5     4                                    
        60    1    0   0  5    5     4                                    
        30    1    0   0  3    5     4                                    
Comparative                                                               
        125   0    0   0  0    1     0                                    
Compound D                                                                
        60    0    0   0  0    0     0                                    
        30    0    0   0  0    0     0                                    
__________________________________________________________________________
EXAMPLE 23 Preparation of N-(2,4-dichloro-5-(1-hydroxymethylethoxyphenyl)-3,4,5,6-tetrahydrophthalimide (Compound No. 23 (Table 4))
To 50 ml of acetic acid, 3.19 g of 3,4,5,6-tetrahydrophthalic anhydride and4.95 g of 2-(2,4-dichloro-5-aminophenoxy)propanol were added and the mixture was heated to reflux under stirring for 16 hours. After cooling, the solvent was evaporated under reduced pressure and the residue was purified by column chromatography (silica gel, benzene/ethyl acetate=10/1 (v/v)) to obtain 1.42 g of the desired product.
Refractive Index: nD 25 1.5640
1 H-NMR (CDCl3, δppm) 1.22 (3H, d), 1.43-1.92 (4H, m), 2.09-2.72 (4H, m), 3.65 (2H, d), 4.20 (1H, m), 4.37 (1H, br), 6.87 (1H, s), 7.42 (1H, s)
EXAMPLE 24 Preparation of N-(4-chloro-2-fluoro-5-(1-hydroxymethylethoxyphenyl)-3,4,5,6-tetrahydrophthalimide (Compound No. 19 (Table 4))
The same procedure as in Example 23 was repeated except that 2-(2-chloro-4-fluoro 5-aminophenoxy)propanol was used as the aniline derivative to obtain the desired product.
Refractive Index: nD 25 1.5494
1 H-NMR (CDCl3, δppm) 1.25 (3H, d), 1.47-1.94 (4H, m), 2.11-2.67 (4H, m), 3.69 (2H, d), 3.85 (1H, m), 4.33 (1H, br), 6.89 (1H, s), 7.17 (1H, s)
EXAMPLE 25 Preparation of N-(4-chloro-2-fluoro-5-(1-acetoxymethylethoxyphenyl)-3,4,5,6-tetrahydrophthalimide (Compound No. 20 (Table 4))
The same procedure as in Example 23 was repeated except that O-acetyl derivative of 2-(2-chloro-4-fluoro-5-aminophenoxy)propanol was used as theaniline derivative to obtain the desired product.
Refractive Index: nD 1.5410
1 H-NMR (CDCl3, δppm) 1.30 (3H, d), 1.50-1.95 (4H, m), 1.99(3H, s), 2.17-2.63 (4H, m), 4.21 (2H, d), 4.50 (1H, br), 6.90 (1H, s), 7.18(1H, s)
EXAMPLE 26 Preparation of N-(4-chloro-2-fluoro-5-(2-benzyloxy-1-methylethoxyphenyl)-3,4,5,6-tetrahydrophthalimide (Compound No. 21 (Table 4))
The same procedure as in Example 23 was repeated except that 4-chloro-2-fluoro-5-(2-(1-benzyloxypropyl)oxyaniline was used as the aniline derivative to obtain the desired
Refractive Index: nD 25 1.5508
1 H-NMR (CDCl3, δppm) 1.28 (3H, d), 1.64-1.97 (4H, m), 2.23-2.62 (4H, m), 4.40 (2H, m), 4.50 (1H, s), 6.82-7.48 (7H, m)
EXAMPLE 27 Preparation of N-(2,4-dichloro-5-(2-(1-(o-fluorobenzyloxy)propyl)oxy)phenyl-3,4,5,6-tetrahydrophthalimide (Compound No. 22 (Table 4))
The same procedure as in Example 23 was repeated except that 2,4-dichloro-5-(2-(1-o-fluorobenzyloxypropyl)oxy)aniline was used as the aniline derivative to obtain the desired product.
Refractive Index: nD 25 1.5668
1 H-NMR (CDCl3, δppm) 1.42 (3H, d), 1.55-2.08 (4H, m), 2.17-2.70 (4H, m), 4.58 (2H, m), 4.70 (1H, m), 6.70-7.58 (6H, m)
EXAMPLE 28 Test for Evaluation of Effectiveness in Growth Inhibition by Soil Treatment
The same procedure as in Example 21 was repeated except that the compounds tested were Compound No.s 19-23. For comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 10 below.
                                  TABLE 10                                
__________________________________________________________________________
              Herbicidal Effectiveness                                    
        Rate  Barnyard-                                                   
                    Pale  Slender          Phytotoxicity                  
Compound No.                                                              
        (a.i. g/10a)                                                      
              grass smartweed                                             
                          amaranth                                        
                               Velvetleaf                                 
                                     Cocklebur                            
                                           Soybean                        
                                                Wheat                     
                                                    Corn                  
__________________________________________________________________________
19      30    5     5     5    5     5     2    0   0                     
        15    4     5     5    5     5     2    0   0                     
20      30    5     5     5    5     5     3    0   0                     
        15    5     5     5    5     5     3    0   0                     
21      30    5     5     5    5     4     3    0   0                     
        15    5     5     5    4     3     3    0   0                     
22      60    0     3     5    5     5     1    0   0                     
        30    0     3     5    5     4     1    0   0                     
23      60    0     4     5    5     5     1    0   0                     
        30    0     4     5    5     4     1    0   0                     
Comparative                                                               
        60    1     3     4    3     4     2    0   0                     
Compound D                                                                
        30    0     2     3    3     3     1    0   0                     
__________________________________________________________________________
EXAMPLE 29 Test for Evaluation of Effectiveness in Growth Inhibition by Foliage Treatment
The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 19-23. Further, for comparison, the Comparative Compound D described in Example 21 was also tested. The results are shown in Table 11 below.
                                  TABLE 11                                
__________________________________________________________________________
              Herbicidal Effectiveness                                    
                                        Annual                            
        Rate  Barnyard-                                                   
                    Small flower        broadleaved                       
                                               Phytotoxicity              
Compound No.                                                              
        (a.i. g/10a)                                                      
              grass umbrellaplant                                         
                            Bulrush                                       
                                 Monochoria                               
                                        weeds  Rice                       
__________________________________________________________________________
19      30    5     5       4    5      5      1                          
        15    5     5       3    5      5      1                          
20      30    4     5       3    5      5      1                          
        15    4     5       3    5      5      1                          
21      30    4     5       3    5      5      1                          
        15    4     5       3    5      5      1                          
22      60    5     5       0    5      5      0                          
        30    4     4       0    5      5      0                          
23      60    5     5       3    5      5      0                          
        30    5     4       3    5      5      0                          
Comparative                                                               
        60    4     5       4    5      5      3                          
Compound D                                                                
        30    3     5       3    4      5      2                          
__________________________________________________________________________
EXAMPLE 30 Preparation of N-(4-chloro-5-hydroxymethylphenyl)-3,4,5,6-tetrahydrophthalimide (CompoundNo. 24 (Table 5))
To 50 ml of acetic acid, 2.47 g of 3,4,5,6-tetrahydrophthalic anhydride and2.56 g of 4-chloro-5-hydroxymethyl aniline were added and the mixture was heated to reflux under stirring for 16 hours. After cooling, the solvent was evaporated under reduced pressure and the residue was purified by column chromatography (silica gel, benzene/ethyl acetate=10/1 (v/v)) to obtain 1.82 g of the desired product.
m.p.: 77°-79° C.
1 H-NMR (CDCl3, δppm) 1.52-1.98 (4H, m), 2.18-2.61 (4H, m),3.08 (1H, s), 4.72 (2H, s), 6.95-7.57 (3H, m)
EXAMPLE 31 Preparation of N-(2-fluoro-4-chloro-5-cyanophenyl)-3,4,5,6-tetrahydrophthalimide (Compound No. 30 (Table 5))
To 30 ml of thionyl chloride, 1.13 g of N-(2-fluoro-4-chloro-5-aminocarbonylphenyl)-3,4,5,6-tetrahydrophthalimide was added and the mixture was heated to reflux under stirring for 16 hours. After cooling, the solvent was evaporated under reduced pressure and the residue was purified by column chromatography (silica gel, benzene/ethyl acetate=10/1 (v/v)) to obtain 0.63 g of the desired product.m.p.: 160°-162° C.
1 H-NMR (CDCl3, δppm) 1.67-2.10 (4H, m), 2.20-2.70 (4H, m),7.40 (1H, d), 7.60 (1H, d)
EXAMPLE 32 Preparation of Compound No. 25 (Table 5)
The same procedure as in Example 30 was repeated except that 4-chloro-5-((acetyloxy)methyl]aniline was used as the aniline derivative to obtain the Compound No. 25.
m.p.: 100°-101° C.
1 H-NMR (CDCl3, δppm) 1.52-2.03 (4H, m), 2.13 (3H, s), 2.22-2.72 (4H, m), 5.22 (2H, s), 7.03-7.58 (3H, m)
EXAMPLE 33 Preparation of Compound No. 26 (Table 5)
The same procedure as in Example 30 was repeated except that 4-chloro-5-[[1-(ethoxycarbonyl)ethoxy)methyl]aniline was used as the aniline derivative to obtain the Compound No. 26.
m.p.: 77°-79° C.
1 H-NMR (CDCl3, δppm) 1.50-1.96 (4H, m), 2.17-2.65 (4H, m),4.72 (4H, s), 6.78-7.67 (7H, m)
EXAMPLE 34 Preparation of Compound No. 27 (Table 5)
The same procedure as in Example 30 was repeated except that 4-chloro-5-[[1-(ethoxycarbonyl)ethoxy]methyl]aniline was used as the aniline derivative to obtain the Compound No. 27.
Refractive Index: nD 25 1.5512
1 H-NMR (CDCl3, δppm) 1.42 (3H, t), 1.62-2.07 (4H, m), 2.15-2.65 (4H, m), 4.22 (4H, q), 4.70 (2H, s), 7.00-7.63 (3H, m)
EXAMPLE 35 Preparation of Compound No. 28 (Table 5)
The same procedure as in Example 31 was repeated except that N-(4-chloro-5-aminocarbonylphenyl)-3,4,5,6-tetrahydrophthalimide was used to obtain the Compound No. 28.
m.p.:135°-137° C.
1 H-NMR (CDCl3, δppm) 1.58-2.03 (4H, m), 2.15-2.72 (4H, m),7.27-7.83 (3H, m)
EXAMPLE 36 Preparation of Compound No. 29 (Table 5)
The same procedure as in Example 31 was repeated except that N-(4-bromo-5-aminocarbonylphenyl)-3,4,5,6-tetrahydrophthalimide was used to obtain the Compound No. 29.
m.p.:151°-153° C.
1 H-NMR (CDCl3, δppm) 1.62-2.11, (4H, m), 2.18-2.76 (4H, m), 7.37-7.93 (3H, m)
EXAMPLE 37 Preparation of Compound No. 31 (Table 5)
The same procedure as in Example 31 was repeated except that N-(4-trifluoromethyl-5-aminocarbonylphenyl)-3,4,5,6-tetrahydrophthalimide was used to obtain the Compound No. 31.
m.p.: 211°-214° C.
1 H-NMR (CDCl3, δppm) 1.58-2.05 (4H, m), 2.23-2.80 (4H, m),7.57-8.07 (3H, m)
EXAMPLE 38 Test for Evaluation of Effectiveness in Growth Inhibition by Soil Treatment
The same procedure as in Example 21 was repeated except that the compounds tested were Compound Nos. 24-30. For comparison, the Comparative Compound A described in Example 5 was also tested. The results are shown in Table 12 below.
                                  TABLE 12                                
__________________________________________________________________________
              Herbicidal Effectiveness                                    
                             Annual                                       
        Rate  Small flower   broadleaved                                  
                                     Phytotoxicity                        
Compound No.                                                              
        (a.i. g/10a)                                                      
              umbrellaplant                                               
                      Monochoria                                          
                             weeds   Rice                                 
__________________________________________________________________________
24      60    5       5      5       0                                    
        30    4       5      5       0                                    
25      125   5       5      5       0                                    
        60    5       4      5       0                                    
26      30    5       5      3       0                                    
        15    5       5      3       0                                    
27      125   4       5      5       0                                    
        60    4       4      4       0                                    
28      30    5       5      5       0                                    
        15    5       5      5       0                                    
29      30    5       5      5       0                                    
        15    5       5      5       0                                    
Comparative                                                               
        60    5       5      5       3                                    
Compound A                                                                
        30    5       4      5       2                                    
__________________________________________________________________________
EXAMPLE 39 Test for Evaluation of Effectiveness in Growth Inhibition by Foliage Treatment
The same procedure as in Example 5 was repeated except that the compounds tested were Compound Nos. 24, 25, 27-31. Further, for comparison, the Comparative Compound A described in Example 5 was also tested. The resultsare shown in Table 13 below.
                                  TABLE 13                                
__________________________________________________________________________
              Herbicidal Effectiveness                                    
        Rate  Pale  Slender           Phytotoxicity                       
Compound No.                                                              
        (a.i g/10a)                                                       
              smartweed                                                   
                    amaranth                                              
                          Velvetleaf                                      
                                Cocklebur                                 
                                      Soybean                             
                                           Wheat                          
                                               Corn                       
__________________________________________________________________________
24      60    3     5     5     5     1    0   0                          
        30    3     5     5     4     1    0   0                          
25      60    3     5     5     4     0    0   0                          
        30    3     4     5     4     0    0   0                          
27      30    5     5     5     5     2    0   0                          
        15    5     5     5     5     1    0   0                          
28      60    4     5     5     5     1    0   0                          
        30    4     5     5     4     1    0   0                          
29      125   3     5     5     4     0    0   0                          
        60    3     5     5     4     0    0   0                          
30      30    5     5     5     5     1    0   0                          
        15    5     5     5     5     1    0   0                          
31      30    5     5     5     5     2    1   0                          
        15    5     5     5     5     2    0   0                          
Comparative                                                               
        60    3     4     3     4     2    0   0                          
Compound A                                                                
        30    2     3     3     3     1    0   0                          
__________________________________________________________________________

Claims (8)

We claim:
1. A tetrahydrophthalimide derivative of the formula (I): ##STR30## wherein X1 is fluorine and X2 represents halogen, hydrogen or trifluoromethyl; R represents: ##STR31## wherein R1 and R2, which may be the same or different, represent hydrogen or methyl, R3 represents 2-tetrahydrofurfuryl or 3-methyl-1,2,4-oxadizol-5-yl; ##STR32## wherein R4 is hydrogen or methyl, R5 is methyl or benzyl; ##STR33## wherein R8 is hydrogen, acyl or arylalkyl, or a C1 -C4 alkyl substituted with an alkoxycarbonyl group.
2. The tetrahydrophthalimide derivative of claim 1, which is represented by the formula: ##STR34## wherein R1, R2 and R3 represent the same meaning as in claim 1.
3. The tetrahydrophthalimide derivative of claim 1, which is represented by the formula: ##STR35## wherein R4 and R5 represent the same meaning as in claim 1.
4. The tetrahydrophthalimide derivative of claim 1, which is represented by the formula: ##STR36## wherein X3 and X4, the same or different, represent halogen, R8 represent the same meaning as in claim 1.
5. A herbicide composition comprising a herbicidal effective amount of the tetrahydrophthalimide derivative of claim 1 in an agriculturally acceptable carrier.
6. The herbicide composition of claim 5, which comprises a herbicidal effective amount of the tetrahydrophthalimide derivative of claim 2 in an agriculturally acceptable carrier.
7. The herbicide composition of claim 5, which comprises a herbicidal effective amount of the tetrahydrophthalimide derivative of claim 3 in an agriculturally acceptable carrier.
8. The herbicide composition of claim 5, which comprises a herbicidal effective amount of the tetrahydrophthalimide derivative of claim 5 in an agriculturally acceptable carrier.
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US20240300932A1 (en) * 2023-02-23 2024-09-12 Guizhou University N-phenylimine derivative and preparation method and use thereof

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